Pharm

Atovaquone

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Atovaquone, Mepron, Malarone

  • Indications
  1. Human Immunodeficiency Virus (HIV)
    1. Pneumocystis carinii Pneumonia prophylaxis
    2. Pneumocystis carinii Pneumonia treatment
    3. Patients unable to tolerate Bactrim
  2. Malaria Prophylaxis and Treatment (Malarone)
    1. Uncomplicated Plasmodium FalciparumMalaria infection from countries with artemisinin resistance
  3. Babesiosis
  • Contraindications
  1. Creatinine Clearance <30 ml/minute/1.73m2
  2. Pregnancy Category C
  3. Breast Feeding of infants under 11 klb (5 kg)
  1. Prophylaxis: 1500 mg orally daily with food
  2. Treatment: 750 mg orally twice daily with food for 21 days
  • Dosing
  • Malaria (Atovaquone/Proguanil or Malarone)
  1. Adults (one tablet: 250/100 mg)
    1. Prophylaxis: 1 tablet (250 mg/100 mg) orally daily
      1. Start 1-2 days before travel
      2. Stop 7 days after return
    2. Treatment: 4 tablets (1000 mg/400 mg) orally daily for 3 days
  2. Children (over age 1 month; one childrens tablet: 62.5/25 mg, one adult tablet: 250/100 mg)
    1. Weight 5-8 kg
      1. Prophylaxis: 1/2 children's tablet orally daily
      2. Treatment: 2 childrens tablets orally daily
    2. Weight 9-10 kg
      1. Prophylaxis: 3/4 tablet orally daily
      2. Treatment: 3 childrens tablets orally daily
    3. Weight: 11-20 kg
      1. Prophylaxis: 1 childrens tablet (62.5/25 mg) orally daily
      2. Treatment: 1 adult tablet (250 mg/100 mg) orally daily
    4. Weight: 21-30 kg
      1. Prophylaxis: 2 childrens tablets orally daily
      2. Treatment: 2 adult tablets orally daily
    5. Weight: 31-40 kg
      1. Prophylaxis: 3 childrens tablets orally daily
      2. Treatment: 3 adult tablet orally daily
    6. Weight: >40 kg (Adult dose)
      1. Prophylaxis: 1 adult tablet (250 mg /100 mg) orally daily
      2. Treatment: 4 adult tablet orally daily
  • Precautions
  • Poor absorption
  1. Take with food (fatty meal) to ensure absorption
  2. Up to 10% of patients still may not absorb Mepron
  3. Repeat dose if Vomiting occurs within one hour of treatment in adults (within 30 minutes for children)
  4. Tablets may be crushed and mixed with 10 ml water if unable to swallow tablets
  • Efficacy
  • HIV
  1. Not as clinically active as Bactrim
  2. Pneumocystis Pneumonia treatment Failure rate: 17%
    1. Contrast with 6% for Bactrim
  • Adverse effects
  1. Less dose-limiting adverse reactions than Bactrim
    1. Atovaquone: 7%
    2. Bactrim: 20%
  2. Rash
  3. Abdominal Pain
  4. Nausea or Vomiting
  5. Diarrhea
  6. Headache
  7. Mild Liver Function Test abnormalities
  • Drug Interactions
  • Reduced plasma levels of Atovaquone
  1. Tetracycline
  2. Metoclopramide (Reglan)
  3. Rifampin
  • References
  1. (2000) Med Lett Drugs Ther 42(1093):109-12 [PubMed]